公开(公告)号：US20120277256A1

公开(公告)日：2012-11-01

申请号：US13542301

申请日：2012-07-05

申请人： Thomas Piccariello ,  Scott B. Palmer ,  John D. Price ,  Robert Oberlender ,  Mary C. Spencer ,  Michaela E. Mulhare

发明人： Thomas Piccariello ,  Scott B. Palmer ,  John D. Price ,  Robert Oberlender ,  Mary C. Spencer ,  Michaela E. Mulhare

IPC分类号： A61K31/167 ,  C07F3/02 ,  A61K31/417 ,  A61K31/52 ,  A61P29/00 ,  A61P25/06 ,  A61P25/16 ,  A61P25/28 ,  A61P25/00 ,  A61P25/18 ,  A61P35/00 ,  A61P9/12 ,  A61P3/10 ,  A61P25/08 ,  C07F3/04

CPC分类号： A61K31/19 ,  A61K31/46 ,  A61K31/498 ,  A61K31/70 ,  A61K31/7088

摘要： Embodiments of the present disclosure include a coordination complex, comprising a first biologically active moiety, a second biologically active moiety, and a metal, wherein the first biologically active moiety and second biologically active moiety are bound to the metal by covalent coordination bonds, and wherein the first biologically active moiety and second biologically active moiety are different. These complexes may enhance the pharmacodynamic properties of biologically active moieties.

摘要翻译： 本公开的实施方案包括配位络合物，其包含第一生物活性部分，第二生物活性部分和金属，其中第一生物活性部分和第二生物活性部分通过共价配位键与金属结合，并且其中 第一生物活性部分和第二生物活性部分是不同的。 这些配合物可增强生物活性部分的药效学性质。

公开(公告)号：US20110009669A1

公开(公告)日：2011-01-13

申请号：US12701483

申请日：2010-02-05

申请人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Robert Oberlender ,  Thomas Piccariello ,  Bernhard J. Paul ,  Christopher A. Verbicky

发明人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Robert Oberlender ,  Thomas Piccariello ,  Bernhard J. Paul ,  Christopher A. Verbicky

IPC分类号： C07C231/12

CPC分类号： A61K31/27 ,  A61K31/165 ,  A61K47/542 ,  C07C237/06 ,  Y10S436/901 ,  Y10T436/173845

摘要： The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

摘要翻译： 本发明描述了使用包含与苯丙胺共价连接的化学部分的化合物，组合物和方法。 这些化合物和组合物可用于减少或预防滥用和过量安非他明。 这些化合物和组合物特别用于提供某些障碍（例如注意力缺陷多动障碍（ADHD），ADD，发作性睡病和肥胖）的耐药性替代治疗。 苯丙胺的口服生物利用度维持在治疗有用的剂量。 在较高剂量下，生物利用度显着降低，从而提供减少口服滥用责任的方法。 此外，本发明的化合物和组合物通过肠胃外途径（例如静脉内或鼻内给药）降低苯丙胺的生物利用度，进一步限制其滥用责任。

公开(公告)号：US20100240601A1

公开(公告)日：2010-09-23

申请号：US12788073

申请日：2010-05-26

申请人： Thomas Piccariello ,  John D. Price ,  Robert A. Oberlender ,  Michaela E. Mulhare ,  Mary C. Spencer ,  Scott B Palmer

发明人： Thomas Piccariello ,  John D. Price ,  Robert A. Oberlender ,  Michaela E. Mulhare ,  Mary C. Spencer ,  Scott B Palmer

IPC分类号： A61K31/7048 ,  C07C259/06 ,  A61K31/166 ,  A61P35/00 ,  A61P25/08 ,  C07H9/04 ,  C07F15/04 ,  A61K31/295

CPC分类号： C07F15/045 ,  A61K31/165 ,  A61K31/166 ,  A61K31/295 ,  A61K31/351 ,  A61K31/4422 ,  A61K31/7048 ,  A61K45/06 ,  A61K47/55 ,  C07F3/00 ,  C07F3/003 ,  C07F3/02 ,  C07F3/06 ,  C07F15/02 ,  C07F15/04 ,  C07H17/02

摘要： A coordination complex having a physiologically acceptable pKa includes a metal and a biologically active agent. The pKa of the coordination complex is less than the pKa of the biologically active agent. A pharmaceutical solution for treating a patient includes a coordination complex and water, wherein the coordination complex is at least partially soluble in the water at physiological pH and in a therapeutically efficacious concentration. A method for treating a patient includes administering a pharmaceutical solution including a coordination complex and water to a patient in need of a biologically active agent.

摘要翻译： 具有生理上可接受的pKa的配位络合物包括金属和生物活性剂。 配位络合物的pKa小于生物活性剂的pKa。 用于治疗患者的药物溶液包括配位络合物和水，其中所述配位络合物在生理pH和治疗有效浓度下至少部分地可溶于水。 用于治疗患者的方法包括向需要生物活性剂的患者施用包括配位复合物和水的药物溶液。

公开(公告)号：US20100197798A1

公开(公告)日：2010-08-05

申请号：US12756773

申请日：2010-04-08

申请人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Robert Oberlender ,  Thomas Piccariello ,  Bernhard J. Paul ,  Christopher A. Verbicky

发明人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Robert Oberlender ,  Thomas Piccariello ,  Bernhard J. Paul ,  Christopher A. Verbicky

IPC分类号： A61K31/165

CPC分类号： A61K31/165 ,  A61K47/542 ,  C07C237/06 ,  Y10S436/901 ,  Y10T436/173845

摘要： The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

公开(公告)号：US07723305B2

公开(公告)日：2010-05-25

申请号：US12202003

申请日：2008-08-29

申请人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Robert Oberlender ,  Thomas Piccariello ,  Bernhard J. Paul ,  Christopher A. Verbicky

发明人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Robert Oberlender ,  Thomas Piccariello ,  Bernhard J. Paul ,  Christopher A. Verbicky

IPC分类号： A61K38/00 ,  A61K51/00 ,  A61K31/785 ,  G01N33/53 ,  G01N33/00

CPC分类号： A61K31/165 ,  A61K47/542 ,  C07C237/06 ,  Y10S436/901 ,  Y10T436/173845

摘要： The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

公开(公告)号：US07713936B2

公开(公告)日：2010-05-11

申请号：US12201907

申请日：2008-08-29

申请人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Robert Oberlender ,  Thomas Piccariello ,  Bernhard J. Paul ,  Christopher A. Verbicky

发明人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Robert Oberlender ,  Thomas Piccariello ,  Bernhard J. Paul ,  Christopher A. Verbicky

IPC分类号： A61K38/00 ,  A61K51/00 ,  A61K31/785 ,  G01N33/53 ,  G01N33/00

CPC分类号： A61K31/165 ,  A61K47/542 ,  C07C237/06 ,  Y10S436/901 ,  Y10T436/173845

摘要： The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

公开(公告)号：US07687466B2

公开(公告)日：2010-03-30

申请号：US12201794

申请日：2008-08-29

申请人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Robert Oberlender ,  Thomas Piccariello ,  Bernhard J. Paul ,  Christopher A. Verbicky

发明人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Robert Oberlender ,  Thomas Piccariello ,  Bernhard J. Paul ,  Christopher A. Verbicky

IPC分类号： A61K38/00 ,  A61K51/00 ,  A61K31/785 ,  G01N33/53 ,  G01N33/00

CPC分类号： A61K31/165 ,  A61K47/542 ,  C07C237/06 ,  Y10S436/901 ,  Y10T436/173845

摘要： The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

公开(公告)号：US07662788B2

公开(公告)日：2010-02-16

申请号：US12201866

申请日：2008-08-29

申请人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Robert Oberlender ,  Thomas Piccariello ,  Bernhard J. Paul ,  Christopher A. Verbicky

发明人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Robert Oberlender ,  Thomas Piccariello ,  Bernhard J. Paul ,  Christopher A. Verbicky

IPC分类号： A61K38/00 ,  A61K51/00 ,  A61K31/785 ,  G01N33/53 ,  G01N33/00

CPC分类号： A61K31/165 ,  A61K47/542 ,  C07C237/06 ,  Y10S436/901 ,  Y10T436/173845

摘要： The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

公开(公告)号：US07655630B2

公开(公告)日：2010-02-02

申请号：US12201760

申请日：2008-08-29

申请人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Robert Oberlender ,  Thomas Piccariello ,  Bernhard J. Paul ,  Christopher A. Verbicky

发明人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Robert Oberlender ,  Thomas Piccariello ,  Bernhard J. Paul ,  Christopher A. Verbicky

IPC分类号： A61K38/00 ,  A61K51/00 ,  A61K31/785 ,  G01N33/53 ,  G01N33/00

CPC分类号： A61K31/165 ,  A61K47/542 ,  C07C237/06 ,  Y10S436/901 ,  Y10T436/173845

摘要： The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

公开(公告)号：US20090306228A1

公开(公告)日：2009-12-10

申请号：US11933846

申请日：2007-11-01

申请人： Travis Mickle ,  Suma Krishnan ,  James Scott Moncrief ,  Christopher Lauderback ,  Thomas Piccariello ,  Randal Kirk

发明人： Travis Mickle ,  Suma Krishnan ,  James Scott Moncrief ,  Christopher Lauderback ,  Thomas Piccariello ,  Randal Kirk

IPC分类号： A61K47/16 ,  C07C229/00

CPC分类号： C07C229/00 ,  A61K47/542

摘要： The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.